Development and Optimization of Floating Microspheres in Amethopterin

Due to the complexity of gastric emptying, as well as its considerable variability, the in vivo efficacy of drug delivery devices cannot be predicted. When it pertains to drugs with an absorption window in the upper small intestine, a controlled drug delivery system with a longer residence period in the stomach may be of considerable practical significance. Recent developments have shown that floating microspheres are particularly well suited for mixing sustained and delayed releases to achieve a variety of release models with a minimal risk of dumping. The aim of present investigation is to develop and analyze the floating microspheres of amethopterin, which after oral administration could increase the gastric residence time and enhance the bioavailability of the drug by sustained release and minimize the dose dependent side effects as well as improves patient compliance. Floating microspheres of ethyl cellulose, Polyvinyl alcohol and polyvinyl pyrrolidone-K90 were formulated by emulsification solvent evaporation technique. The various parameters of prepared microspheres were studied for SEM, flow properties, buoyancy, yield, percent drug loading, in vitro dissolution studies, stability in different pH and FTIR studies. Microspheres prepared with different concentrations of polymers were spherical in shape with smooth surface. The size of microspheres was in range of 256.02 µm and 362.84 µm. Good drug entrapment and buoyancy were observed for formulation F2. The in vitro drug release after 6h was found to be in range from 58.15% to 96.28%. It was established that the newly created floating microspheres of Amethopterin provide an appropriate and practical solution for the sustained release of medication over a longer period of time, resulting in increased oral bioavailability, effectiveness, as well as better patient compliance.

Formulation and in-vitro Evaluation of Carvedilol Gastroretentive Capsule as (Superporous Hydrogel)

The preferred route of drug administration is the oral route, but drugs with narrow absorption window in the gastrointestinal tract are still challenging. The ability to extend and monitor the gastric emptying time is a valuable tool for processes remaining in the stomach longer than other traditional dosage forms. The purpose of this study was to formulate and evaluate gastroretentive superporous hydrogel (SPH) of carvedilol with view to improve its solubility and increase gastric residence time in order to get sustained release formulas via utilization of various kinds and concentrations of hydrophilic polymers then after, incorporate the best prepared formula into capsules. Sixteenth formulae of SPH hybrid were prepared by gas blowing technique from the following materials; monomers (Poly vinyl alcohol, and Acrylamide), cross-linkers (Methylene bisacrylamide, and glutaraldehyde), hybrid agent (Chitosan), foaming agent (NaHCO3) and foam stabilizer (Tween 80). Different amounts or concentrations of these materials were utilized to investigate their effect on SPH properties (density, porosity, floating, drug content, drug release, swelling time, and swelling ratio). The soaking procedure was utilized for loading of carvedilol into SPH hybrid (6.25mg/2.5g SPH). After analysis the results statistically and application the similarity factor (f2) equation, formula F8 was selected as the best formula and incorporated into capsules. The drug release data were applied to different mathematical kinetics and the results were shown to be fitted to Higuchi model and the release mechanism was (non fickian) diffusion. The overall results suggested that the proposed SPH hybrid drug delivery system is encouraging for carvedilol specific delivery to the stomach.

Development and characterization of effervescent floating tablet of famotidine for treatment of peptic ulcer

Floating drug delivery systems (FDDS) are utilized to target drug discharge in the stomach or to the upper parts of intestine. Famotidine has been the most extensively used drug for the management of peptic ulcer for various decades. The current study concerns the development and evaluation of floating tablets of famotidine which, after oral administration, are planned to extend the gastric residence time, enhance drug bioavailability and aim the gastric ulcer. A FDDS was expanded using gas-forming agents, like sodium bicarbonate, citric acid and hydrocolloids, like hydroxypropyl methylcellulose (HPMC) and carbopol 934P. The prepared tablets were evaluated in terms of their pre-compression parameters, physical characteristics, buoyancy, buoyancy lag-time, in vitro release, and swelling index. The formulations were optimized for the different viscosity grades of HPMC, carbopol 934P and its concentrations and combinations. The consequences of the in vitro release studies demonstrated that the optimized formulation (F6) could sustain drug release (98%) for 24 h and remain buoyant for 24 hr. Optimized formulation (F6) showed no considerable change in physical appearance, drug content, total buoyancy time or in vitro dissolution study after storage at 40°C/75% RH for 3 months. Lastly the tablet formulations establish to be economical and may conquer the draw backs associated with the drug during its absorption. Keywords: Famotidine, Floating drug delivery system, Hydrocolloids, Gastric residence time.

Formulation And Evaluation Of Floating Microspheres Of Cefdinir

Various approaches have been used to retain the dosage form in the stomach as a way ofincreasing the gastric residence time (GRT), including floatation systems; high-density systems; mucoadhesive systems; magnetic systems; unfoldable, extendible, or swellable systems; andsuperporous hydrogel systems. The aim of this study was to prepare and evaluate floatingmicrospheres of cefdinir for the prolongation of gastric residence time. Themicrospheres were prepared byCapillary Extrusion method.A full factorial design was applied to optimize the formulation. The optimum batch of microsphere exhibited smooth surfaces with good flow and packing properties, prolonged sustained drug release, remained buoyant for more than 12 hrs, high entrapment efficiency upto68%.Scanning electron microscopy confirmed the hollown structure with particle size in the order of190 μm. The studies revealed that increase in concentration of gum Karaya increased the drug release from the floating microspheres.

Floating Microsphere of Curcumin as Targeted Gastro-retentive Drug Delivery System

Microspheres carrier system made from natural or synthetic polymers used in sustained release drug delivery system. The present study involves formulation and evaluation of floating microspheres of Curcumin for improving the drug bioavailability by prolongation gastric residence time. Curcumin, natural hypoglycemic agent is a lipophilic drug, absorbed poorly from the stomach, quickly eliminated and having short half-life so suitable to formulate floating drug delivery system for sustained release. Floating microspheres of curcumin were formulated by solvent evaporation technique using ethanol and dichloromethane (1:1) as organic solvent and incorporating various synthetic polymers as coating polymer, sustain release polymers and floating agent. The final formulation were evaluated various parameters such as compatibility studies, micrometric properties, In-vitro drug release and % buoyancy. FTIR studies showed that there were no interaction between drug and excipients. The surface morphology studies by SEM confirmed their spherical and smooth surface. The mean particles size were found to be 416-618µm, practical yield of microspheres was in the range of 60.21±0.052% - 80.87±0.043%, drug entrapment efficiency 47.4±0.065% - 77.9±0.036% and % buoyancy 62,24±0.161% - 88.63±0.413%. Result show that entraptmency increased as polymer (Eudragit RS100) conc. Increased. The drug release after 12 hrs. was 72.13% - 87.13% and it decrease as a polymer (HPMC, EC) concentration was decrease.

FORMULATION AND CHARACTERIZATION OF CLARITHROMYCIN FLOATING TABLETS BY USING VARIOUS POLYMERS

The present study outlines a systematic approach for designing and development of Clarithromycin floating tablets to enhance the bioavailability and therapeutic efficacy of the drug. Floating tablets of Clarithromycin have shown sustained release there by proper duration of action at a particular site and are designed to prolong the gastric residence time after oral administration. Different formulations were formulated by using direct compression technique. A floating drug delivery system (FDDS) was developed by using sodium bicarbonate as gas-forming agent and Chitosan, HPMC K4M and Ethyl cellulose as polymers. The preformulation parameters like Organoleptic properties, angle of repose, bulk density, tapped density, Hausners ratio, carrs index and compressibility index of pure drug was evaluated and complied with the pharmacopoeial specifications. FTIR studies showed there was no interaction between drug and polymer. The prepared tablets were evaluated in terms of their physical characteristics, post compression parameters in vitro release and buoyancy lag time the results of the in vitro release studies showed that the optimized formulation (C7) could sustain drug release for 12 hrs by using Ethyl cellulose in the concentration of 50 mg. The in vitro drug release followed Kors Mayer peppas release. Results revealed that the floating formulation of the Clarithromycin is the best formulation to obtain better therapeutic effect and Ethyl cellulose at a concentration of 50mg up to some extent it increases the Bioavailability of the drug to retain the dosage form on the desired site for effective period of the time.

Preparation of Acyclovir-Containing Solid Foam by Ultrasonic Batch Technology

In recent years, the application of solid foams has become widespread. Solid foams are not only used in the aerospace field but also in everyday life. Although foams are promising dosage forms in the pharmaceutical industry, their usage is not prevalent due to decreased stability of the solid foam structure. These special dosage forms can result in increased bioavailability of drugs. Low-density floating formulations can also increase the gastric residence time of drugs; therefore, drug release will be sustained. Our aim was to produce a stable floating formula by foaming. Matrix components, PEG 4000 and stearic acid type 50, were selected with the criteria of low gastric irritation, a melting range below 70 °C, and well-known use in oral drug formulations. This matrix was melted at 54 °C in order to produce a dispersion of active substance and was foamed by different gases at atmospheric pressure using an ultrasonic homogenizer. The density of the molded solid foam was studied by the pycnometer method, and its structure was investigated by SEM and micro-CT. The prolonged drug release and mucoadhesive properties were proved in a pH 1.2 buffer. According to our experiments, a stable foam could be produced by rapid homogenization (less than 1 min) without any surfactant material.

FORMULATION AND EVALUATION OF FLOATING IN SITU GEL OF OMEPRAZOLE MAGNESIUM FOR ORAL DRUG DELIVERY SYSTEM

Objective: Omeprazole magnesium is indicated for the treatment of erosive esophagitis associated with gastroesophageal reflux disease. It is one of the highly prescribed proton pump inhibitor in the management of peptic ulcer diseases. The therapeutic concentration of a drug in blood can be maintained for a prolonged period of time by administering it in the form of in situ floating gel dosage form. Omeprazole magnesium undergoes degradation at a low pH of the esophagus and stomach; it is therefore given as in situ gel, so, there is minimum contact with acidic pH. Methods: Omeprazole magnesium suspension prepared using various polymers and floating agents in varying concentrations. Several evaluation tests including dissolution test to ensure the release of the drug from formulation by in vitro technique, color and homogeneity, in vitro floating duration, in vitro gelling capacity, drug content determination, pH of the formulation, and floating lag time were studied. Results: All formulations demonstrated good Fourier-transform infrared compliance and no interaction between drug, polymer, and other excipients. The study’s findings show that the formulation F6 showed the best results. Conclusion: The developed formulation was a viable alternative conventional solution by virtue of its ability to enhance bioavailability through its longer gastric residence time and ability to sustain drug release as well as the advantage of floating and pH which minimize the degradation of omeprazole magnesium which is easily degraded by acidic environment.